Composition
Active ingredients:
Ebastine 20 mg.
Auxiliary substances:
gelatin – 13.00 mg,
mannitol-9.76 mg,
aspartame-2.00 mg,
mint flavor-2.00 mg
Pharmacological action
Pharmacodynamics
Long – acting histamine H1-receptor blocker. Prevents histamine-induced smooth muscle spasms and increased vascular permeability.
After taking the drug inside, the pronounced anti-allergic effect begins in 1 hour and continues for 48 hours. After a 5-day course of treatment with Kestine® lyophilized tablets 20 mg, antihistamine activity persists for 72 hours due to the action of the active metabolite.
With prolonged use, a high level of blockade of peripheral histamine H1 receptors remains without the development of tachyphylaxine. The drug does not have a pronounced anticholinergic and sedative effect.
There was no effect of Kestine® 20 mg lyophilized tablets on the ECG QT interval at a dose of 100 mg exceeding the recommended daily dose (20 mg) by 5 times.
Pharmacokinetics
Suction
After oral use, it is rapidly absorbed and almost completely metabolized in the liver, turning into the active metabolite of carbastine. After a single dose of 20 mg of the drug, the maximum concentration of carbastine in blood plasma is reached in 1-3 hours and averages 157 ng / ml. Fatty foods accelerate the absorption of carbastine (blood concentration increases by 50%) and presystemic metabolism (formation of carbastine).
Distribution
With daily use of the drug, the equilibrium concentration is reached in 3-5 days and is 130-160 ng / ml. Binding to plasma proteins of Ebastine and carbastin is more than 95%.
The elimination
of T1 / 2 of carbastine is from 15 to 19 hours. 66% of the drug is excreted as conjugates by the kidneys.
Pharmacokinetics in special clinical cases
In elderly patients, the pharmacokinetic parameters do not change significantly.
With renal insufficiency, T1 / 2 increases to 23-26 hours, and with hepatic insufficiency-up to 27 hours, but the concentration of the drug does not exceed therapeutic values.
Indications
Allergic rhinitis of various etiologies (seasonal and/or year-round).
Urticaria of various etiologies, including chronic idiopathic.
Use during pregnancy and lactation
It is contraindicated to use the drug during pregnancy and lactation (breastfeeding).
Contraindications
- Hypersensitivity to the components of the drug;
- phenylketonuria;
- pregnancy and lactation (breastfeeding):
- children under 15 years of age;
- hypersensitivity to the components of the drug.
Caution: use in patients with prolonged QT interval, hypokalemia, renal and / or hepatic insufficiency.
Side effects
From the nervous system: from 1% to 3.7% – headache, drowsiness; less than 1% – insomnia.
From the digestive system: from 1% to 3.7% – dryness of the oral mucosa; less than 1% – dyspepsia, nausea, abdominal pain.
From the respiratory system: less than 1% – sinusitis, rhinitis.
Other: less than 1% – asthenic syndrome; possible allergic reactions.
Interaction
It is not recommended to use Kestine® tablets lyophilized 20 mg simultaneously with ketoconazole and erythromycin (increased risk of prolongation of the QT interval).
Kestine ® lyophilized tablets 20 mg does not interact with theophylline, indirect anticoagulants, cimetidine, diazepam, ethanol and ethanol-containing drugs.
How to take, course of use and dosage
The drug is intended for resorption in the oral cavity, regardless of food intake.
Adults, children and adolescents over 15 years of age: appoint 20 mg (1 lyophilized tablet) 1 time / day. The course of treatment is determined by the disappearance of symptoms of the disease.
No dose adjustment is required in elderly patients.
No dose adjustment is required in patients with impaired renal function.
With minor to moderate hepatic insufficiency, the drug can be used in the usual dose. In severe hepatic impairment, the daily dose of Ebastinee 10 mg should not be exceeded.
Special precautions for handling the product
Overdose
Symptoms: moderate effects on the central nervous system (fatigue) and autonomic nervous system (dryness of the oral mucosa) can occur only at high doses (300-500 mg, which is 15-25 times higher than the therapeutic dose).
Treatment: in case of overdose, gastric lavage, monitoring of vital body functions, and symptomatic treatment are recommended. There is no specific antidote for abastine.
Special instructions
Ebastine may distort the results of skin allergy tests. Therefore, it is recommended to conduct such tests no earlier than 5-7 days after discontinuation of the drug.
Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention
In the event of side effects from the central nervous system, a minimal decrease in the ability of patients to drive vehicles and engage in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions is possible.
Form of production
Freeze-dried tablets
Storage conditions
Keep out of reach of children at a temperature not exceeding 25°C.
Shelf
life is 3 years.
Active ingredient
Abastin
Dosage form
Tablets
Description
Children over 12 years old, For adults
Indications
Urticaria, Allergic Rhinitis, Allergic Conjunctivitis, Allergy
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Side effects of Kestine, lyophilized pills 20mg, 10pcs.
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